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PROTAC

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The PROTAC molecule itself contains three distinct portions: a ligand for binding to the target protein, a ligand for binding to an E3 ligase, and a linker joining these two ligands.

PROTACs (proteolysis-targeting chimaeras) are bifunctional molecules that bring a target protein into spatial proximity with an E3 ubiquitin ligase to trigger target ubiquitination and subsequent proteasomal degradation. Effective redirection of ligase poly-ubiquitination activity toward a new substrate protein requires formation of a ligase:PROTAC:target ternary complex, an intermediate species that is crucial to the cellular activity of degrader molecules. A characteristic feature of PROTACs mode of action is their sub-stoichiometric catalytic activity that alleviates the requirement for target engagement and occupancy of traditional inhibitors. New PROTAC molecules designed guided by the crystal structure show exquisite selectivity for inducing cellular depletion of Brd4 over its BET family members Brd2 and Brd3.

Products Related to PROTAC(273)

  • GC81732 structure
    GC81732iAfaPhos1
    Purity: >98%

    iAfaPhos1 is a FKBP12F36V epimer ligand.

  • GC81862 structure
    GC81862YJ1206 TFA
    Purity: >98.00%

    YJ1206 TFA is an orally active selective CDK12 / CDK13 PROTAC degrader.

  • GC81882 structure
    GC81882PROTAC CARM1 degrader-1 TFA
    Purity: >98.00%

    PROTAC CARM1 degrader-1 TFA is a highly selective CARM1 PROTAC degrader, with a DC 50 of 8.1 nM in MCF‑7 cells.

  • GC91440 structure
    GC91440Dth
    Purity: >95.00%

    Dth est une chimère de ciblage de protéolyse (PROTAC) composée de la sonde fluorescente pour l'ARN DFHBI et du composé immunomodulateur thalidomide.

  • GC91442 structure
    GC91442C-02
    Purity: >95.00%

    C-02 est une chimère de ciblage de protéolyse (PROTAC) composée de l'inhibiteur d'hexokinase lonidamine lié au ligand cereblon thalidomide.

  • GC91582 structure
    GC91582Pomalidomide 4'-PEG5-amine (hydrochloride)
    CAS: 2357117-23-6
    Purity: >95.00%

    Pomalidomide 4’-PEG5-amine is a PEGylated form of the cereblon (CRBN) inhibitor pomalidomide .

  • GC91584 structure
    GC91584Pomalidomide 4'-alkylC6-amine (hydrochloride)
    CAS: 2375194-37-7
    Purity: >98.00%

    Pomalidomide 4'-alkylC6-amine is a building block in the synthesis of proteolysis-targeting chimeras (PROTACs) and a derivative of the cereblon inhibitor pomalidomide .

  • GC91586 structure
    GC91586PROTAC RAF Degrader 1
    CAS: 2413035-41-1
    Purity: >98.00%

    PROTAC RAF degrader 1 is a proteolysis-targeting chimera (PROTAC) that contains the inhibitor of mutant V600E and wild-type B-RAF vemurafenib (PLX4032; ) conjugated to VHL ligand 1 .

  • GF04054 structure
    GF04054PROTAC CDK9 degrader-4
    CAS: 2411021-01-5
    Purity: >95.00%

    PROTAC CDK9 degrader-4 is a PROTAC protein degrader that targets CDK9 (cyclin-dependent kinase 9).